摘要:
Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).
摘要:
A compound of formula 1′ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要:
The present invention relates to compounds of formula 1 wherein the groups X, Ra, Rb, R1, R1′, R2, R2′, R2″, R2′″, V and n may have the meanings given in the claims and in the specification, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要翻译:本发明涉及式1的化合物,其中基团X,R a,R b,R 1,R 1, R 2,R 2,R 2,R“2”,R“2”,R“2” ,V和n可以具有权利要求书和说明书中给出的含义,以及其作为药物组合物的用途,特别是用于治疗炎性和阻塞性呼吸道疾病。
摘要:
Compounds of the formula I wherein n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.
摘要:
The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要:
A compound of formula 1′″ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R2′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要:
A compound of formula 1′ wherein: V is —CH2—, —NH—, or —O—; Ra and Rb are each independently hydrogen, C1-4-alkyl, or halogen-C1-4-alkyl, or Ra and Rb together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R1 and R1′ are each independently hydrogen, C1-6-alkyl, C3-6-cycloalkyl, halogen-C1-6-alkyl, halogen-C3-6-cycloalkyl, or C1-6-alkylene-C3-6-cycloalkyl, or R1 and R1′ together are a C2-5-alkylene bridge wherein one or more hydrogen atoms are optionally replaced by halogen; R2, R2′, R2″, and R′″ are each independently hydrogen, C1-6-alkyl, halogen-C1-6-alkylene, OH, HO—C1-6-alkylene, —O—C1-6-alkyl, C6-10-aryl, C6-10-aryl-C1-4-alkylene, C6-10-aryl-C1-6-alkylene-O, COOH, COOC1-6-alkyl, O—C1-6-alkylene-COOH, O—C1-6-alkylene-COOC1-6-alkyl, NHSO2—C1-6-alkyl, CN, NH2, NH—C1-6-alkyl, N(C1-6-alkyl)2, NO2, S—C1-6-alkyl, SO2—C1-6-alkyl, SO—C1-6-alkyl, O(CO)C1-6-alkyl, COC1-6-alkyl, NHCOC1-6-alkyl, or halogen; and n is 0, 1, or 2, or an optical isomer thereof, or a corresponding acid addition salt thereof with a pharmacologically acceptable acid, and the use thereof as pharmaceutical compositions, particularly for the treatment of inflammatory and obstructive respiratory complaints.
摘要:
This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.
摘要:
The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
摘要:
This invention relates to novel sulfoximine substituted quinazoline derivatives of formula I wherein Ar, R1 and R2 are as defined herein, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.